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Evotec

Recent Posts

SLC Transporter Substrate Identification Fact Sheet

Posted by Evotec on Jan 26, 2023 10:38:59 AM

Learn more about the human SLC transporter substrate identification assay including:

  • Background information
  • Assay details and protocol summary
  • Data generated in the SLC transporter substrate identification assay
DOWNLOAD

Tags: Fact Sheets, ADME/DMPK

PBMC Proliferation Fact Sheet

Posted by Evotec on Jan 26, 2023 10:35:31 AM

Learn more about our PBMC proliferation assay including:

  • Background information
  • Assay details and protocol summary
  • Data generated in the PBMC proliferation assay
DOWNLOAD

Tags: Fact Sheets, Toxicology & Safety

P-gp Substrate Identification Fact Sheet

Posted by Evotec on Jan 26, 2023 10:21:28 AM

Learn more about the P-gp substrate identification assay including:

  • Background information
  • Assay details and protocol summary
  • Data generated in the P-gp substrate identification assay
DOWNLOAD

Tags: Fact Sheets, ADME/DMPK

Comparing Basic Static Models for Predicting Clinical CYP3A4 Induction Risk

Posted by Evotec on Jan 19, 2023 12:08:48 PM

Drug-drug interaction (DDI) studies are an important part of the regulatory drug development process. The US FDA, EMA and Japanese PMDA have issued guidance on the conduct of these DDI studies, however, a harmonised guidance is currently under review (ICH M12) and is expected to be adopted in April 2024. The risk of DDI can be assessed in vitro and data analysed using models of varying complexity.  As identifying potential safety issues is the main purpose of these studies, many of the models have been developed to over-estimate the risk of DDI .This, however, needs to be balanced with the risk of false positives and the potential of unnecessary clinical DDI studies which are expensive and time consuming to perform. It is essential, therefore, to choose the most accurate model when analysing data from in vitro DDI studies.   

In this poster, we focus on:

  • an evaluation of the various models for predicting clinical CYP3A4 induction risk from in vitro data
  • a comparison of basic R3 values (with and without a scaling factor) with correlation methods (relative induction score (RIS) and Imax/EC50 values)

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK

Ultra-fast LC-MS/MS in DMPK Screening

Posted by Evotec on Jan 19, 2023 10:43:07 AM

LC-MS/MS produces highly sensitive, specific and reproducible data, however, throughput can be a limitation and this can lead to a bottleneck in sample analysis from pharmacokinetic (PK) studies.

In this poster, we focus on:

  • the development of ultra-fast separation chromatography to improve efficiency of sample analysis in small molecule PK studies
  • a comparison of the rapid separation method with conventional column technology for the analysis of plasma and blood samples from a PK study

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK

Echo MS in High Throughput ADME

Posted by Evotec on Jan 18, 2023 6:55:44 PM

The Echo® MS system, developed by Sciex, uses Acoustic Ejection Mass Spectrometry (AEMS). This chromatography-free technology generates sample droplets and introduces small reproducible volumes of 2.5nL (scalable to 25nL with multiple injections) to the mass spectrometer via an Open Port Interface with minimal carryover. It not only reduces sample requirements, it also facilitates dramatic increases in throughput with the potential to run 1 second cycle times. Despite these advantages, current potential limitations include reduced sensitivity compared to conventional LC-MS/MS and interference due to lack of separation.

In this poster, we focus on:

  • the evaluation of the Echo® MS technology for its application in routine ADME screening
  • a comparison of the Echo® MS with established, routine LC-MS/MS methods for the analysis of samples generated from microsomal stability and cytochrome P450 (CYP) inhibition assays

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK

BioSeed 2023

Posted by Evotec on Jan 13, 2023 6:35:08 PM

Date: 23 January 2023

Venue: County Hall, London, UK

Attendees: Florence Eustache, David Pardoe

 

bioseed2023

 

Evotec is an Industry Sponsor at BioSeed 2023, the early-stage life sciences investment event, organised by OBN.

 

Our Senior Vice President, Head of Global Molecular Architects, David Pardoe and Vice President Business Development, Florence Eustache will make a keynote presentation on:

The AI paradigm shift: Just a flash in the pan or here to stay?

 

If you wish to meet with us in London, get in touch via the form below, we will be happy to arrange a meeting.

Learn more about BioSeed 2023

Tags: Events, Evotec

Keystone Symposia

Posted by Evotec on Jan 5, 2023 3:46:12 PM

Date: 15 - 19 January 2023

Location: Keystone Resort, CO

 

Jeremie Boucher, Evotec's SVP, Head of Metabolic Disease, will present at the Keystone Symposia on 'Adipose Tissue: Energizing Good Fat' in Colorado, United States. Jeremie's discussion “Adipose Tissue Targets in Metabolic Disease” will cover several different potential therapeutic targets or pathways in adipose tissue, to treat #metabolicdiseases

Discover more about the event

Tags: Events

JP Morgan Healthcare Conference 2023

Posted by Evotec on Jan 5, 2023 3:41:49 PM

Date: 9 - 12 January 2023

Location: San Francisco, CA

 

 Our experts, Jon Gunther and Nathalie Joly, will be available on site to discuss your drug discovery and R&D requirements. Get in touch via the Biotech Showcase partneringONE app or via email - info@evotec.com

Tags: Events

The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile

Posted by Evotec on Dec 2, 2022 10:31:14 AM

The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent

This publication details the discovery of a series of selective agonists for Transient Receptor Potential Melastatin 5 (TRPM5) culminating with the identification of a lead compound.

Gastrointestinal (GI) disease including inflammatory bowel disease (ulcerative colitis and Crohn’s disease), and GI motility disorders (neuropathic constipation (NC), and gastroparesis) are serious life limiting conditions for patients. TRPM5 is a non-selective monovalent cation channel activated by intracellular Ca2+ increase which, within the GI system, plays a critical role of propagating the signal through membrane depolarization and initiating the release of Interleukin (IL)-25 and other paracrine factors. We hypothesized that a TRPM5 agonist will activate the release of IL-25 and non-neuronal ACh, leading to improvement in motility through a prokinetic mechanism.

In the paper we describe: 

  • The process of our discovery starting from a high throughput screening hit through to the identification of a lead compound
  • The selectivity of the lead compound versus related family members TRPA1, TRPV1, TRPV4, TRPM4 and TRPM8
  • The drug metabolism and pharmacokinetics (DMPK) profile of the lead compound
  • The in vivo efficacy of lead compound in a mouse model of gastrointestinal motility

READ NOW

Tags: Articles & Whitepapers, In vitro Biology, Metabolic Disease & Complications